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Letters in Organic Chemistry, Volume 1, No. 3, 2004

 

Contents

 

Influence of the Nature of Low Valent Titanium Reagents in McMurry Olefination: Stereoselective Synthesis of Symmetrical and Unsymmetrical Hydroxystilbenes Pp.203-207

Narayan V. Mayekar, Subrata Chattopadhyay and Sandip K. Nayak

[Abstract]

 

Catalytic Enantioselective Addition of Me2Zn to Aromatic Aldehydes Promoted by New Modular Thiophene-Oxazoline Ligands Pp.208-211

P. G. Cozzi and M. Locatelli

[Abstract]

 

Yb(OTf)3 and ZrCl4 Mediated Rearrangement of Alkoxybenzyl Allyl Ethers into Aldehydes#Pp.212-214

Palakodety Radha Krishna, Ch. Govardhan Reddy and G. V. M. Sharma

[Abstract]

 

Synthesis of Alicyclic β-lactams via the Ugi Reaction on a Solid Support Pp.215-220

S. Gedey, J. Van der Eycken and F. Fulop

[Abstract]

 

Intramolecular Azide Cycloaddition enroute to the New Pyrrolo[2,1-c][1,2,3] triazolo[1,5-a][1,4]benzodiazepine Skeleton Pp.221-223

G. Broggini, I. De Marchi, M. Martinelli, G. Paladino and A. Penoni

[Abstract]

 

Re-Evaluation of a Solid-Phase Hydantoin Synthesis Pp.224-226

Jesus Vazquez, Miriam Royo and Fernando Albericio

[Abstract]

 

Multivalent Recognition of Flavin Derivatives Using Polymer Scaffolds Pp.227-230

Joseph B. Carroll, Mark Gray, Kevin M. Bardon, Hiroshi Nakade and Vincent M. Rotello

[Abstract]

 

Synthesis of Luminescent N-Arylcarbazoles by Copper Bronze-Mediated Reaction Pp.231-237

M. Martinez-Palau, E. Perea, F. Lopez-Calahorra and D. Velasco

[Abstract]  

 

Synthesis of Boronated Alkoxyphenylalanines Pp.238-245

A. Wolan, A. Laczynska, Z. Rafinski and M. Zaidlewicz

[Abstract]

 

Synthesis of Enol Adenosine 5'-Phosphate Derivatives by the Perkow Reaction of a Silylated Adenosine 5'-Phosphonate Derivative with α-Halo Ketones Pp.246-248

Tomohisa Moriguchi, Kazuhisa Okada, Kohji Seio and Mitsuo Sekine

[Abstract]

 

Chiral Linker 1. A Novel Chiral Auxiliary Derived from m-Hydrobenzoin as Enantiomerically Pure Linker for Solid Phase Organic Chemistry Pp.249-253

P. Gaertner, C. Schuster and M. Knollmueller

[Abstract]

 

Chemoenzymatic Approach to a (R)-3, 4-Diaminobutanoic Acid Derivative with a Suitable Orthogonal Protection for Solid Phase Peptide Synthesis Pp.254-256

Monica Lopez-Garcia, Ignacio Alfonso and Vicente Gotor

[Abstract]

 

Further Advances in the Synthesis of α,β’-Difunctionalised Pyrroles Pp.257-260

Severine Hebbe and Luc Dechoux

[Abstract]

 

Efficient Synthesis of Octahydro-5H-Dibenz[b,f]azepin-10-one Derivatives by an Easy Two-Step Route from Available 2-Carbethoxymethyl Cyclohexanone and Anilines Pp.261-263

Alirio Palma, Jacqueline Jaimes Barajas, Vladimir V. Kouznetsov, Elena Stashenko, Ali Bahsas and Juan Amaro-Luis

[Abstract]

 

Mild and Most Efficient Silylcyanation of Aldehydes Catalyzed by Cesium Fluoride Pp.264-267

Sung Soo Kim and Dae Ho Song

[Abstract]

 

Highly Diastereoselective Methylation of Five-Ring N,O-Acetals Pp.268-270

Martin Brunner, Thomas Straub, Pauli Saarenketo, Kari Rissanen and Ari M. P. Koskinen

[Abstract]

 

The First Dye-sensitized Photooxygenation of 2-(C-glycosyl)furans. One-Pot Stereoselective Approach to New Carbohydrate Derivatives Pp.271-275

Flavio Cermola, M. Rosaria Iesce and Stefania Montella

[Abstract]

 

A Facile Synthesis of Dibenzylated p-tert-Butylcalix[4]Crowns Under Non-Diluted Reaction Conditions Pp.276-279

Hirohito Tsue, Tatsuya Takimoto, Rui Tamura, Chieko Kikuchi and Shunitz Tanaka

[Abstract]

 

Collapse and Self-Reconstruction of Mesoscopic Architectures of Supramolecular J Aggregates in Solution: From Strings to Tubular Rods Pp.280-287

Hiroshi Yao, Chris A. Michaels, Stephan J. Stranick, Takeshi Isohashi and Keisaku Kimura

[Abstract]

 

Abstracts

 

[Back to top] Influence of the Nature of Low Valent Titanium Reagents in McMurry Olefination: Stereoselective Synthesis of Symmetrical and Unsymmetrical Hydroxystilbenes

Narayan V. Mayekar, Subrata Chattopadhyay and Sandip K. Nayak

 

Intramolecular reductive deoxygenation of ethylenedioxy tethered symmetrical and unsymmetrical aromatic bis(ketone) ethers with the low-valent titanium (LVT) reagent (TiCl4-Zn-DME) yielded the corresponding cyclic stilbenes with excellent Z-selectivity. On the other hand, coupling of the aldehydic tethered ethers proceeded with high E-selectivity with the LVT reagent (TiCl3/Li/KCl (2.0 eq.) /THF). Dealkylation of the cyclic stilbenes furnished the geometrically pure hydroxystilbenes.

 

[Back to top] Catalytic Enantioselective Addition of Me2Zn to Aromatic Aldehydes Promoted by New Modular Thiophene-Oxazoline Ligands

P. G. Cozzi and M. Locatelli

 

A small library of aryl and dialkyl 3-hydroxy thiophene 2-oxazolines was simply prepared by direct and selective metalation of 4-tertbutyl-2-(thiophene-2-yl)-4,5-dihidrooxazole and its successive reaction with aromatic and aliphatic ketones. The ligand 7h was able to promote the addition of Me2Zn to aromatic aldehydes with good enantioselectivity (up to 92 % ee).

 

[Back to top] Yb(OTf)3 and ZrCl4 Mediated Rearrangement of Alkoxybenzyl Allyl Ethers into Aldehydes#

Palakodety Radha Krishna, Ch. Govardhan Reddy and G. V. M. Sharma

 

Lewis acid mediated rearrangement of alkoxybenzyl allyl ethers into aldehydes in moderate to good yields, catalysed either by Yb(OTf)3 or ZrCl4 is reported. The ZrCl4 catalysed transformation offers mild and easily adaptable clean reaction conditions and good yields of the products. Additionally, ZrCl4 catalysed rearrangement under solvent free conditions is an advantageous modification.

 

[Back to top] Synthesis of Alicyclic β-lactams via the Ugi Reaction on a Solid Support

S. Gedey, J. Van der Eycken and F. Fulop

 

Via the Ugi 4-centre 3-component reaction (U-4C-3CR), bicyclic cis-2-azetidinone derivatives were synthetised from cyclic β-amino acids on Super Acid Sensitive Resin (Sasrin). 2-, 3- or 4-Formylbenzoic acid was immobilised on the resin through its carboxy function. The U-4C-3CR was also carried out in solution, making use of scavenger resins for purification.

 

[Back to top] Intramolecular Azide Cycloaddition enroute to the New Pyrrolo[2,1-c][1,2,3] triazolo[1,5-a][1,4]benzodiazepine Skeleton

G. Broggini, I. De Marchi, M. Martinelli, G. Paladino and A. Penoni

 

The unknown pyrrolo[2,1-c][1,2,3]triazolo[1,5-a][1,4]benzodiazepin-8-one ring system has been synthesised starting from the N-Boc-L-proline methyl ester. The totally diastereoselective intramolecular 1,3- dipolar cycloaddition of the azide 9 constitutes the key step of the synthetic sequence.

 

[Back to top] Re-Evaluation of a Solid-Phase Hydantoin Synthesis

Jesus Vazquez, Miriam Royo and Fernando Albericio

 

Solid-phase methods for the preparation of hydantoins are reviewed. Furthermore, an optimized method based on the concourse of 1,1’-carbonyldiimidazole allows the preparation of hydantoins without loss of chiral integrity.

 

[Back to top] Multivalent Recognition of Flavin Derivatives Using Polymer Scaffolds

Joseph B. Carroll, Mark Gray, Kevin M. Bardon, Hiroshi Nakade and Vincent M. Rotello

 

Random copolymers of polystyrene were functionalized with diamidopyridine and anthracene recognition elements. Cooperative recognition between isobutyl flavin "guest" molecules and mixed recognition unit modified "host" copolymers was observed arising from a combination of aromatic stacking and hydrogen bonding interactions.

 

[Back to top] Synthesis of Luminescent N-Arylcarbazoles by Copper Bronze-Mediated Reaction

M. Martinez-Palau, E. Perea, F. Lopez-Calahorra and D. Velasco

 

A copper bronze-mediated carbazole arylation reaction under mild reaction conditions is reported. Yields of 9-arylcarbazoles achieved are nearly quantitative and almost independent of the nature of the substitution on the carbazole or the aryl halide. A series of 9-arylcarbazole derivatives have been synthesized and their luminescence studied.

 

[Back to top] Synthesis of Boronated Alkoxyphenylalanines

A. Wolan, A. Laczynska, Z. Rafinski and M. Zaidlewicz

 

Synthesis of (2-methoxy-5-dihydroxyborylphenyl)alanine, (2-butoxy-5-dihydroxyborylphenyl) alanine, and (2-methoxy-4-dihydroxyborylphenyl)alanine for Boron Neutron Capture Therapy is described. In the key step, the amino acid functionality was introduced by the Wittig reaction. The approach provides a general access to alkoxy substituted boronated phenylalanines.

 

[Back to top] Synthesis of Enol Adenosine 5'-Phosphate Derivatives by the Perkow Reaction of a Silylated Adenosine 5'-Phosphonate Derivative with α-Halo Ketones

Tomohisa Moriguchi, Kazuhisa Okada, Kohji Seio and Mitsuo Sekine

 

This paper deals with the synthesis of α-substituted enol ester derivatives of adenosine 5’-phosphate. These compounds were formed by the Perkow reaction of α-chloromethyl ketones with an in situgenerated adenosine-5'-yl bis(trimethylsilyl) phosphite intermediate. Among these reactions, the use of α- chloro-2',4'-difluoroacetophenone gave predominantly the enol phosphate derivative over the Arbuzov reaction product and the carbonyl adduct, which were formed as byproducts.

 

[Back to top] Chiral Linker 1. A Novel Chiral Auxiliary Derived from m-Hydrobenzoin as Enantiomerically Pure Linker for Solid Phase Organic Chemistry

P. Gaertner, C. Schuster and M. Knollmueller

 

The synthesis and utility of a novel, m-hydrobenzoin derived chiral auxiliary in stereoselective α-alkylation reactions using convenient solution chemistry as well as the attachment of an analogous system onto a solid support and its application as a dual chiral auxiliary and linker is described.

 

[Back to top] Chemoenzymatic Approach to a (R)-3, 4-Diaminobutanoic Acid Derivative with a Suitable Orthogonal Protection for Solid Phase Peptide Synthesis

Monica Lopez-Garcia, Ignacio Alfonso and Vicente Gotor

 

The efficient chemoenzymatic synthesis of a (R)-3,4-diaminobutanoic acid derivative has been achieved. The final compound has suitable orthogonal protection for solid phase peptide synthesis.

 

[Back to top] Further Advances in the Synthesis of α,β’-Difunctionalised Pyrroles

Severine Hebbe and Luc Dechoux

 

The reactivity of pyrrololactone 3 towards reductive and alkylating agents has been studied and the synthesis of diverse α, β’-difunctionalised pyrroles is presented. The ambivalent reactivity of compound 3 towards the different nucleophilic reagents has been rationalised.

 

[Back to top] Efficient Synthesis of Octahydro-5H-Dibenz[b,f]azepin-10-one Derivatives by an Easy Two-Step Route from Available 2-Carbethoxymethyl Cyclohexanone and Anilines

Alirio Palma, Jacqueline Jaimes Barajas, Vladimir V. Kouznetsov, Elena Stashenko, Ali Bahsas and Juan Amaro-Luis

 

Synthesis of new octahydrodibenz[b,f]azepin-10-one derivatives by a two-step synthetic route based on 2-carbethoxymethyl cyclohexanone reactivity is reported.

 

[Back to top] Mild and Most Efficient Silylcyanation of Aldehydes Catalyzed by Cesium Fluoride

Sung Soo Kim and Dae Ho Song

 

Cesium fluoride (CsF) catalyzes the addition of trimethylsilyl cyanide (TMSCN) to various aldehydes. Aromatic, aliphatic, cyclic and heterocyclic aldehydes have been converted into the corresponding trimethylsilyl ethers. Most of the aldehydes show over 99% yield for 20min. The mechanism of silylcyanation has been proposed.

 

[Back to top] Highly Diastereoselective Methylation of Five-Ring N,O-Acetals

Martin Brunner, Thomas Straub, Pauli Saarenketo, Kari Rissanen and Ari M. P. Koskinen

 

Highly diastereoselective methylation of (2S,4S)- and (2R,4S)-3-tert-butyl 4-methyl 2-tertbutyloxazolidine-3,4-dicarboxylate (1a/b) is reported. The relative and absolute configuration of the methylated products was assigned by NOESY and confirmed by a crystal structure of 1a.

 

[Back to top] The First Dye-sensitized Photooxygenation of 2-(C-glycosyl)furans. One-Pot Stereoselective Approach to New Carbohydrate Derivatives

Flavio Cermola, M. Rosaria Iesce and Stefania Montella

 

The singlet oxygen oxygenation of 2-(α-C-glucopyranosyl)furans 1 leads readily and diastereoselectivity to the corresponding endoperoxides 2 whose fate can be controlled. Compounds 2 thermally rearrange into cis-dicarbonyl-α-O-glucosides 3 while by reduction they afford the cis-C-analogs 5. The latter readily convert to trans-8, which by silica gel chromatography tautomerize into β-anomers 9.

 

[Back to top] A Facile Synthesis of Dibenzylated p-tert-Butylcalix[4]Crowns Under Non-Diluted Reaction Conditions

Hirohito Tsue, Tatsuya Takimoto, Rui Tamura, Chieko Kikuchi and Shunitz Tanaka

 

The straightforward synthesis of calix[4]crown derivatives in excellent yields under non-diluted reaction conditions is described. The reactions proceed smoothly at ordinary temperature and substrate concentrations of up to 1 M. Theoretical calculations on the reaction intermediates indicate that preorganization originating from the coordination of oxygen atoms to sodium ions plays an important role in the reaction.

 

[Back to top] Collapse and Self-Reconstruction of Mesoscopic Architectures of Supramolecular J Aggregates in Solution: From Strings to Tubular Rods

Hiroshi Yao, Chris A. Michaels, Stephan J. Stranick, Takeshi Isohashi and Keisaku Kimura

 

This Letter reports the collapse and subsequent self-reassembly of mesoscopic architectures of supramolecular J aggregates in solution. Ultrasonication of the string-like 5,5'-dichloro-3,3'-disulfopropyl thiacyanine (TC) J aggregates caused fragmentation (collapse) of the initial morphology, followed by a prompt self-reconstruction into mesoscopic rod-like architectures. Fluorescence microscopy, polarized light microscopy, atomic force microscopy and near-field scanning optical microscopy revealed that the apparent rod-like morphology was a tubular architecture with a monomolecular wall (single-wall) and open ends.